269results about How to "High drug loading rate" patented technology

The invention discloses a macromolecular microcarrier and a preparation method thereof, belonging to the technical field of biomedicine. The preparation method comprises the following steps of: splitting a silk solution and a drug solution into micrometer grade liquid drops with core-shell structures under the action of a high-voltage electric field by adopting a coaxial high-voltage electrostatic technology and a freeze drying method; concreting through liquid nitrogen, and then preparing the microcarrier which is difficult to dissolve in water through freeze drying. The microcarrier is in the shape of a microsphere with the core-shell structure, and the diameter of the microsphere is 100-500 micrometers; the shell of the microcarrier comprises the components of silk fibroin; the random-coil conformation of silk fibroin molecules is 80-90 percent; the shell is in a porous structure, and an aperture is 5-20 micrometers; and a core of the microcarrier comprises the components of water-soluble drugs. The silk microcarrier has extensive application prospect in the fields of cell culture, drug release, and the like.

The invention relates to a preparation and application of a new macromolecule lipidosome. The structure is a vesicle which has a lipide dual-layer structure containing duoparental chitosan longchain alkyl quaternary ammonium salt as well as phospholipid with micromolecule. The chitosan longchain alkyl quaternary ammonium salt is characterized in that: the weight average molar mass is bigger than 2000; the chitosan longchain alkyl quaternary ammonium salt can be dissolved in chloroform and other organic solvent, which contains carboxyl, amino or quaternary ammonium salt radical and concretely is one of the duoparental chitosan longchain alkyl quaternary ammonium salt disclosed by 200710056993.4 of China Invention Patent. The surface of the macromolecule lipidosome can be connected with various Liver-Targeted preparations. The macromolecule lipidosome can carry water-soluble, oil-dissolving or duoparental materials including medicine, protein, gene, nutrition, vitamin, magnetic granule and quantum dot, etc. The macromolecule lipidosome has the advantages of high wrapping rate, simple and convenient operation, strong applicability and low cost; the macromolecule lipidosome after being covered has even distributed granule diameter which can be lower than 20nm for the smallest, has stable system and strong functions for carrying medical tiny balls and slowly controlling as well as releasing.

The invention discloses a sustained-release pesticide composition and a pesticide preparation and a preparation method thereof. The sustained-release pesticide composition comprises a graphene nanometer material and pesticide active ingredients, wherein the weight of the pesticide active ingredients is 0.1% to 60% of the total weight of the pesticide preparation, and the remainder includes the graphene nanometer material and a pesticide acceptable carrier. The pesticide preparation provided by the invention adopts graphene and derivatives thereof as pesticide carriers, and the pesticide active ingredients are supported on the surface of the graphene material by physical adsorption, thereby improving the light stability of the pesticide, realizing the effective control of the pesticide release time, and increasing the pesticide loading amount.

The invention relates to a preparation method of a difunctional mesoporous silicon ball composite targeted drug delivery system, and belongs to the field of nanobiomedicine. The method comprises the steps that a coprecipitation method is adopted for preparing superpara magnetism Fe3O4 nanoparticles, then, hexadecyl trimethyl ammonium bromide is used as a template, a photosensitizer is doped, accordingly, the surfaces of the magnetic nanoparticles and the photosensitizer are wrapped by a layer of mesoporous silica, covalent linkage and physical absorption of anti-cancer medicine are achieved, finally, surface modification is carried out through folic acid and hyaluronic acid, and the difunctional mesoporous silicon ball composite targeted drug delivery system is obtained. According to the system, multiple effects of nuclear magnetism radiography, fluorescence imaging, magnetic hyperthermia, photoactive therapy and chemotherapy are integrated, diagnosis and treatment are integrated, magnetic targeting and FA/HA dual receptor-mediated targeting effect can more effectively enhance the targeting combination of the medicine and tumor cells, the effective concentration of the medicine in the tumor parts is improved, effect enhancement and toxicity reduction are achieved, the killability for the cancer cells is enhanced through dual drug loading, and the treatment effect on tumors is remarkably improved. The product obtained through the preparation method has a quite large application prospect in the field of medicine control release.

The invention provides a sophora davidii anthocyanin crude extract and further provides a microcapsule of the sophora davidii anthocyanin crude extract. The anthocyanin crude extract prepared by the invention has good antioxidant activity, so that further purification on anthocyanin is avoided, and the production and use cost is reduced. The invention provides the microcapsule, aiming at the problem that the anthocyanin as a main component is difficult to widely use in existing food because the anthocyanin is easy to oxidate and degrade under the action of illumination, high temperature and oxygen and cannot be dissolved in liposoluble substances, a microencapsulation technique which is used for keeping the stability of the anthocyanin and extending the application range thereof is provided, the tolerance for heat, light and the like is increased, and the stability is obviously increased.

The invention discloses self-setting calcium phosphate micro spheres, a method for preparing the same and application thereof. The preparation method comprises the following steps of: mixing glutin and deionized water to obtain solution of glutin; mixing polysaccharide gum and deionized water to obtain solution of polysaccharide gum; mixing completely dissolved solution of glutin and solution of polysaccharide gum to obtain solution of glutin/polysaccharide gum; fully mixing the solution of glutin/polysaccharide gum and calcium phosphate cement by stirring to obtain pasty self-setting calciumphosphate slurry, fully dispersing the self-setting calcium phosphate slurry into soybean oil by stirring, removing the soybean oil by filtration, and repeatedly washing the micro spheres by acetone and alcohol to obtain the wet micro spheres; and performing curing hydration and drying of the wet micro spheres to obtain the self-setting calcium phosphate micro spheres. The method has the advantages that: the sintering treatment of the micro spheres is unnecessary, medicaments, growth factors or other active (functional) components can be synchronously loaded in the preparation process, the grain size of the obtained self-setting calcium phosphate micro spheres is 0.12 to 2.61mm, and the obtained self-setting calcium phosphate micro spheres are not disintegrated in 6 to 32 hours.

The invention discloses a swelling-type hollow silk fibroin micro-needle drug delivery system and a preparation method thereof. According to the technical scheme of the preparation method, a swelling modified silk fibroin solution is casted in a PDMS mold to be vacuumized, dried and molded as a hollow needle-type housing. After that, a silk fibroin micro-needle array provided with cavities in the hollow needle-type housing is filled with powder-like or solution-like drugs, vacuumizing and drying are carried out to form a drug part. Finally, a layer of modified silk fibroin solution is cast, dried and molded as a cladded coating. The cladded coating is removed to obtain the swelling-type hollow silk fibroin micro-needle drug delivery system. The drugs are wrapped inside the cavities of the silk fibroin micro-needle arrays, so that the system is high in drug loading ratio and low in skin allergenicity and stimulation. The system facilitates the sustained release and the controlled release of micro-needle drugs. Meanwhile, according to the preparation method, since the swelling modified silk fibroin solution is cast, dried and molded in a mild processing condition, the system is low in processing cost and suitable for large-scale production. Drugs are directly wrapped in the cavities of the swelling hollow micro-needles, so that controlled-release drugs are swelled in the micro-needle base material. In this way, the biological activities of the controlled-release drugs are maintained, while the structure of the hollow silk fibroin micro-needle drug delivery system is greatly simplified. The system is better in practicality.

The invention relates to a method for using template nanometer self-assemble technique to prepare polypeptide oral microcapsule, which comprises: using polypeptide grain as template grain; using two biological compatible macromolecules with reversed charges as wall material; based on mutual attraction between different charges, combining the macromolecule materials from layer to layer, to form thin protective film on the surface of polypeptide grain, to obtain the polypeptide microcapsule. The invention is stable in acid medium, but releases polypeptide medicine in neutral medium, to keep the function of polypeptide grain in oral. And the polypeptide microcapsule can be dispersed into water or other liquid to form variable micro nanometer polypeptide oral liquid; or mixing the micrometer or sub-micron polypeptide microcapsule to form sheets, ejections, etc.

The invention relates to a lactoferrin chitosan particle preparation method, in particular to a nanoscale lactoferrin chitosan particle preparation method and aims to solve problems of large particle size and low encapsulation efficiency and drug loading ratio of existing lactoferrin chitosan particles. The method includes: firstly, preparing chitosan solution, lysozyme mixed liquid and lactoferrin solution; secondly, adding the lysozyme mixed liquid into the chitosan solution, shaking, and boiling to obtain modified chitosan solution; thirdly, mixing the lactoferrin solution with the modified chitosan solution, stirring, adding sodium tripolyphosphate and stirring; fourthly, centrifuging to obtain precipitates which are the lactoferrin chitosan particles. Chitosan oligosaccharide prepared according to the method is conducive for bodies to absorb and high in bioactivity, protonic amino groups are easier to expose and crosslink with phosphate groups as compared with long-chain chitosan molecules, and accordingly binding degree of a drug loading system is raised. In addition, the encapsulation efficiency reaches 30%, the drug loading ratio reaches 26%, and the lactoferrin chitosan particles are used for preparation of lactoferrin medicines for oral administration.

The invention belongs to the field of preparation of targeted therapeutic microspheres of slow release formulation and in particular relates to a preparation method of taxol-loading polylactic acid-hydroxyacetic acid (PLGA) microspheres. The preparation method comprises the following steps: dissolving a polylactic acid-hydroxyacetic acid copolymer in an organic solvent, and adding a taxol drug, wherein the polymer and the taxol drug are uniformly dissolved to obtain an organic phase; dropwise adding the organic phase into a fresh polyvinyl alcohol aqueous solution and curing and forming microspheres; and performing centrifugal separation on the cured drug-loading microspheres to obtain the uniformly dispersed taxol-loading polylactic acid-hydroxyacetic acid (PLGA) microspheres. The taxol-loading targeted therapeutic PLGA microspheres prepared by the preparation method have an ideal drug loading ratio and encapsulation efficiency while guaranteeing the drug stability of taxol, can reach an effect of slow release, maintain the optimum drug concentration in vivo, prolong the action time of the drug and reduce the side effects brought by burst release of the drug, and have important theoretical value and actual application prospect.

The invention relates to a preparation method of camptothecin drug slow release microcapsule. Firstly, camptothecin drug microcrystal is positioned into deionized water for ultra sonic dispersion, secondly, the dispersed camptothecin drug microcrystal is positioned into polycation solution for adsorption, centrifugation and washing, third, the camptothecin drug microcrystal adsorbing the polycation is positioned into polyanion solution for adsorption, centrifugation and washing, then the step two and the step three are repeated, and thereby the drug microcapsule with core-shell structure is obtained. The microcapsule is very stable, can realize controlled release of the drug, can be produced to be micron-nanometer drug oral liquid or injection, and also can be produced to be drug capsule, and tablets, etc. The process of the invention is simple, the reaction condition is mild, the operation is easy, the reproducibility is good, the environment is protected, the invention provides substantial foundation and technical support for the application and the research of the camptothecin and other drugs having the characteristics of high curative effect, but large toxicity and poor water solubility, and has good application prospect.

The invention relates to the field of preparation of porous microspheres, in particular to porous microspheres for medicine carriers, a preparation method and a medicine loading method. The method comprises the following steps of: 1) dissolving a degradable di-block amphiphilic polymer material in an organic solvent to form an oil phase O; 2) adding the oil phase O into a water phase W which contains a stabilizing agent to form O/W pre-emulsion; 3) allowing the O/W pre-emulsion obtained in the step 2 to pass through a microporous membrane to obtain O/W emulsion; and 4) removing the organic solvent from the emulsion obtained in the step 3, and curing, performing centrifugal washing and freeze drying to obtain porous medicine carrying microspheres. The organic solvent in the step 1) at least comprises a solvent of which the solubility in water is less than 2 percent; and the volume ratio of the oil phase O to the water phase W is 1:5-20. The porous microspheres overcome the problem thatthe conventional sustained release microspheres cannot be completely released at a later stage, and can effectively keep the medicine activity in the processes of carrying, storing and releasing the medicines.

The invention discloses a preparation method of embolic microspheres containing ion exchange functional groups. According to the preparation method, AMPS (2-acrylamide-2-methylpro panesulfonic acid) is prepared into a mild crosslinking prepolymer and then blended with SA (sodium alginate), a PAMPS and SA polymer blend solution is added into liquid paraffin, interpenetrating polymer network microspheres prepared with a reversed phase suspension crosslinking method are in regular spherical shape, the particle sizes range between 300 microns and 700 microns in a concentrated manner, the drug loading rate of the microspheres can be 25%-45%, the performance after high temperature sterilization and sealing is stable, and the embolic microspheres have application prospect in anti-tumor embolism chemotherapy.

The invention discloses a narcotic analgesic-loaded sustained-release microsphere and a preparation method thereof and application thereof. The narcotic analgesic-loaded sustained-release microspherecan be continuously released for 1 to 7 days, the burst release rate is less than 20% within 0.5 hour, and the drug embedding rate is higher than 80%, so that high drug embedding rate and low burst release rate and sustained release can be realized. The method has simple process, the obtained product has uniform particle size, batches of products have good repeatability, and the preparation methodis easy for industrial production.

The invention discloses a preparation method of porous high-swelling gelatin microspheres. The preparation method comprises the following steps: preparing gelatin into a water solution with the mass concentration of 30%, adding another component as a pore-foaming agent, wherein the pore-foaming agent can be an inorganic substance such as nano calcium carbonate powder as well as a water-soluble high polymer such as polyethylene glycol, polyvinyl alcohol, polymethylacrylic acid-2-(N,N-dimethyl) amino ethyl ester, uniformly mixing the water solution of gelatin with the pore-foaming agent, suspending and dispersing in paroline, adding a spann-80 and tween-60 mixed stabilizer, slowly dropwise adding a formaldehyde solution while stirring, reacting for hours so that the gelatin is crosslinked; then, filtering and separating microspheres, removing the pore-foaming agent, purifying and drying, thus obtaining the porous high-swelling gelatin microspheres. When the microspheres are used as a medicine-carrying embolic agent, the medicine carrying rate and the medicine carrying speed of medicines can be increased, and the use performance is improved.

The invention relates to a taxol nano targeting slow-release long-circulating liposome and a preparation method thereof. The taxol nano targeting slow-release long-circulating liposome of the invention mediates the structure of polyethylene glycol modificatory chitosan derivative by folate receptor; and the invention utilizes the chitosan derivative as an auxiliary material to prepare a novel taxol preparation by a reverse phase evaporation method or film dispersion method, and the prepared taxol nano targeting slow-release long-circulating liposome has the grain size smaller than 100nm, can freely run in the blood, penetrates the endothelial cell of a target tissue, can be uptaken by a tumor cell to enter the cell, releases the contained taxol in the cell, and greatly improves the utilization efficiency of medicaments. In addition, the surface of the prepared taxol nano targeting slow-release long-circulating liposome is also covered by a layer of polyethylene glycol (PEG) which can prolong the dwell time of liposome in the blood, reduce the uptaken amount of liposome by liver and spleen reticuloendothelial systems, and is beneficial to the absorption of tumor tissues and lesion parts.

The invention relates to a multi-layer composite dual-drug-loaded microsphere as well as a preparation method and an application thereof in preparing antineoplastic drugs. In a preferred preparation method, the multi-layer composite dual-drug-loaded microsphere is mainly composed of two model drugs, chitosan and glucan; according to the preparation method, a chitosan microsphere self-assembled template is prepared by virtue of a double-emulsification-crosslinking method, then on the basis of an electrostatic interaction between polyelectrolytes having different charges, the glucan is adsorbed on the surface of the chitosan microsphere so as to form a glucan/chitosan dual-layer composite drug-loaded microsphere, and based on an electrostatic adsorption interaction between the chitosan and the glucan on the surface of the dual-layer composite drug-loaded microsphere, the chitosan/glucan/chitosan multi-layer composite dual-drug-loaded microsphere is formed. An in vitro release test on the multi-layer composite dual-drug-loaded microsphere having pH responsivity provided by the invention shows that the multi-layer composite dual-drug-loaded microsphere has a good sustained-release effect, and an in vitro antineoplastic cell activity test shows that the multi-layer composite dual-drug-loaded microsphere has a good inhibitory effect.

The invention discloses a method for preparing sustained-release microgranules. The method includes steps of 1), preparing solid dispersion of biodegradable and biocompatible water-insoluble polymer and water-soluble drug; 2), dissolving the prepared solid dispersion in an organic solvent C to form solid dispersion emulsion; 3), injecting the obtained solid dispersion emulsion into oil solution with surfactants to form uniform emulsion; 4), curing microgranules in the emulsion by means of solvent evaporation or solvent extraction, and collecting, washing and drying the microgranules to obtain the sustained-release microgranules. The invention further discloses the sustained-release microgranules prepared by the aid of the method and application of the sustained-release microgranules to implantable sustained-release pharmaceutical compositions. The method, the sustained-release microgranules and the application have the advantages that full procedures for preparing the sustained-release microgranules by the aid of the method are carried out at the normal temperature or the low temperatures, and accordingly the method is quite favorable for preparing polymer matrix compositions from high-temperature-sensitive drugs; excellent similarly zero-level sustained-release effects can be realized by the prepared sustained-release microgranules, and the drugs are stable in concentration in sustained-release period.

The invention discloses a water-soluble wood fire retardant and a preparation method thereof. The water-soluble wood fire retardant comprises, by mass, 30-50% of a phosphorus-containing compound, 20-40% of an amino compound, 10-30% of a boron-containing compound, 5-15% of an aluminum salt, and 0.5-3% of a surfactant. The water-soluble wood fire retardant contains high content of P, N, B and Al elements, is an efficient halogen-free fire retardation system formed by compounding P, N, B, Al and the surfactant, fully performs the fire retardant soup surface tension reduction, infiltrating depth increase and drug load rate increase of the surfactant, can be easily dissolved in water, and can be directly processed to prepare the above fire retardant soup in order to realize wood fire retardation drug load treatment. The method is simple, and the water-soluble wood fire retardant has the advantages of good wood fire retardation treatment effect, no migration or moisture absorption phenomenon, low cost, corrosion and insect resistance of wood, and dimensional stability.

A medicine carried polycyanoacrylate nanoparticle as medicine carrier with high covering percentage is prepared through dissolving medicine in the cyanoacrylate monomers, and fine emulsion polymerizing reaction.